α,β-不饱和酰胺酯、二乙基亚磷酸吡啶甲酯及其顺式铂（II）配合物的体外烷基化反应
In vitro alkylating of alpha, beta-unsaturated amidoesters, diethyl pyridylmethylphosphonates and their cis-Pt(II)complexes.
作者信息
Najman-Bronzewska L, Ochocki J
机构信息
Department of Pharmaceutical Chemistry and Drug Analysis, Medical University, Lódz, Poland.
出版信息
Pharmazie. 1997 Mar;52(3):198-202.
The alkylating ability of alpha,beta-unsaturated amidoesters 1a-8d, diethyl pyridylmethylphosphonate esters and their cis-platinum(II) complexes has been investigated based on the test with 4-(4'-nitrobenzyl)pyridine (NBP) (Preussmann Test). Of the compounds tested for alkylating activity, only cis-platinum(II) phosphonate complexes were found to possess activity. The highest activity was found for CiS-[PtCl2(4-pmpe)2] where 4-pmpe is diethyl 4-pyridylmethylphosphonate. The results show a correlation between alkylating activity in vitro and cytotoxic activity in vivo for platinum(II) complexes.
基于4-(4'-硝基苄基)吡啶（NBP）测试（普雷斯曼测试），研究了α,β-不饱和酰胺酯1a - 8d、吡啶基甲基膦酸二乙酯及其顺铂（II）配合物的烷基化能力。在测试的具有烷基化活性的化合物中，仅发现顺铂（II）膦酸配合物具有活性。对于顺式-[PtCl2(4 - pmpe)2]活性最高，其中4 - pmpe是4 - 吡啶基甲基膦酸二乙酯。结果表明，铂（II）配合物的体外烷基化活性与体内细胞毒性活性之间存在相关性。
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